E2F-3 Inhibitors
The chemical class of E2F-3 inhibitors encompasses a diverse array of compounds that directly or indirectly modulate the activity of E2F-3, a pivotal transcription factor crucial for cell cycle regulation. Among the direct inhibitors, palbociclib, roscovitine, and flavopiridol stand out as compounds targeting cyclin-dependent kinases (CDKs). By disrupting the Rb-E2F pathway, these inhibitors inhibit E2F-3-mediated transcription, providing a direct mechanism for regulating cell cycle progression. In addition to these direct inhibitors, compounds such as NU6027, trichostatin A, and GW8510 offer alternative avenues to influence E2F-3 activity indirectly. NU6027, a selective CDK2 inhibitor, impacts the Rb-E2F pathway, emphasizing the central role of CDKs in E2F-3 regulation. Trichostatin A, functioning as a histone deacetylase inhibitor, modulates chromatin structure, thereby influencing E2F-3 binding and subsequent transcriptional regulation. GW8510, another CDK2 inhibitor, disrupts downstream events involving E2F-3, highlighting the versatility of indirect modulation strategies.
Daphnetin, LY294002, and resveratrol add to the repertoire of compounds exhibiting indirect modulation of E2F-3. Daphnetin's impact on the PI3K/AKT pathway influences Rb phosphorylation and downstream events involving E2F-3. LY294002, a PI3K inhibitor, alters the phosphorylation status of Rb, providing another point of intervention in E2F-3 regulation. Resveratrol, a natural compound, affects the SIRT1 pathway, influencing Rb deacetylation and, consequently, E2F-3 activity. These diverse pathways underline the intricate network of signaling cascades involved in the regulation of E2F-3. R547, AZD5438, and AG-024322, as selective CDK inhibitors, further contribute to the comprehensive view of potential strategies for inhibiting E2F-3. Their modulation of the Rb-E2F pathway emphasizes the significance of CDKs as key players in the regulatory cascade governing E2F-3 activity.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Palbociclib | 571190-30-2 | sc-507366 | 50 mg | $321.00 | ||
Palbociclib is a direct inhibitor of CDK4/6, modulating the cell cycle. By inhibiting CDK4/6, it disrupts the Rb-E2F pathway, leading to the inhibition of E2F-3. This inhibition can prevent the transcriptional activation of E2F-3 and subsequent cell cycle progression. | ||||||
Roscovitine | 186692-46-6 | sc-24002 sc-24002A | 1 mg 5 mg | $94.00 $265.00 | 42 | |
Roscovitine is a CDK inhibitor that directly targets multiple CDKs, including CDK2. By inhibiting CDKs, it affects the Rb-E2F pathway, leading to the modulation of E2F-3 activity. This interference can result in the inhibition of E2F-3-mediated transcription and cell cycle progression. | ||||||
Flavopiridol Hydrochloride | 131740-09-5 | sc-207687 | 10 mg | $317.00 | ||
Flavopiridol is a CDK inhibitor that directly targets CDK1, CDK2, and CDK4. By inhibiting these CDKs, it disrupts the Rb-E2F pathway, leading to the inhibition of E2F-3. This interference can prevent the transcriptional activation of E2F-3 and subsequent cell cycle progression. | ||||||
NU6027 | 220036-08-8 | sc-215591 | 10 mg | $156.00 | 1 | |
NU6027 is a selective inhibitor of CDK2, influencing the Rb-E2F pathway. By inhibiting CDK2, it disrupts the downstream events involving E2F-3, leading to the modulation of E2F-3 activity. This interference can result in the inhibition of E2F-3-mediated transcription and cell cycle progression. | ||||||
Trichostatin A | 58880-19-6 | sc-3511 sc-3511A sc-3511B sc-3511C sc-3511D | 1 mg 5 mg 10 mg 25 mg 50 mg | $152.00 $479.00 $632.00 $1223.00 $2132.00 | 33 | |
Trichostatin A is a histone deacetylase (HDAC) inhibitor, indirectly modulating E2F-3. By influencing chromatin structure, it can affect the accessibility of E2F-3 binding sites, leading to altered transcriptional regulation. This modulation highlights the role of epigenetic regulation in controlling E2F-3 activity. | ||||||
GW8510 | 222036-17-1 | sc-215122 sc-215122A | 1 mg 5 mg | $293.00 $626.00 | 8 | |
GW8510 is a selective inhibitor of CDK2, impacting the Rb-E2F pathway. By inhibiting CDK2, it disrupts the downstream events involving E2F-3, leading to the modulation of E2F-3 activity. This interference can result in the inhibition of E2F-3-mediated transcription and cell cycle progression. | ||||||
Daphnetin | 486-35-1 | sc-203022 | 10 mg | $84.00 | ||
Daphnetin is a coumarin derivative that indirectly influences E2F-3 activity. By modulating the PI3K/AKT pathway, it can impact the phosphorylation status of Rb, affecting the downstream events involving E2F-3. This interference can result in the inhibition of E2F-3-mediated transcription and cell cycle progression. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $123.00 $400.00 | 148 | |
LY294002 is a PI3K inhibitor, influencing the PI3K/AKT pathway. By inhibiting PI3K, it can affect the phosphorylation status of Rb, influencing the downstream events involving E2F-3. This interference can result in the inhibition of E2F-3-mediated transcription and cell cycle progression. | ||||||
Resveratrol | 501-36-0 | sc-200808 sc-200808A sc-200808B | 100 mg 500 mg 5 g | $80.00 $220.00 $460.00 | 64 | |
Resveratrol is a natural compound that indirectly modulates E2F-3 activity. By influencing the SIRT1 pathway, it can impact the deacetylation of Rb, affecting the downstream events involving E2F-3. This interference can result in the inhibition of E2F-3-mediated transcription and cell cycle progression. | ||||||
R547 | 741713-40-6 | sc-364596 sc-364596A | 2 mg 5 mg | $375.00 $395.00 | ||
R547 is a selective inhibitor of CDK1, CDK2, and CDK4, impacting the Rb-E2F pathway. By inhibiting these CDKs, it disrupts the downstream events involving E2F-3, leading to the modulation of E2F-3 activity. This interference can result in the inhibition of E2F-3-mediated transcription and cell cycle progression. | ||||||